JP2013526843A5 - - Google Patents
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- JP2013526843A5 JP2013526843A5 JP2012557201A JP2012557201A JP2013526843A5 JP 2013526843 A5 JP2013526843 A5 JP 2013526843A5 JP 2012557201 A JP2012557201 A JP 2012557201A JP 2012557201 A JP2012557201 A JP 2012557201A JP 2013526843 A5 JP2013526843 A5 JP 2013526843A5
- Authority
- JP
- Japan
- Prior art keywords
- inhibitor
- cancer
- raf
- subject
- phosphorylation
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 239000003112 inhibitor Substances 0.000 claims 29
- 230000002401 inhibitory effect Effects 0.000 claims 29
- 201000011510 cancer Diseases 0.000 claims 17
- 102100002306 MAP3K8 Human genes 0.000 claims 16
- 101710039067 MAP3K8 Proteins 0.000 claims 16
- 101700007719 RAF1 Proteins 0.000 claims 14
- 102100016115 RAF1 Human genes 0.000 claims 13
- 239000000126 substance Substances 0.000 claims 13
- 108091000081 Phosphotransferases Proteins 0.000 claims 12
- 102000001253 Protein Kinases Human genes 0.000 claims 12
- 210000004027 cells Anatomy 0.000 claims 12
- 101700069422 ZHX2 Proteins 0.000 claims 11
- 108020004999 Messenger RNA Proteins 0.000 claims 9
- 229920002106 messenger RNA Polymers 0.000 claims 9
- 238000006366 phosphorylation reaction Methods 0.000 claims 9
- 230000000865 phosphorylative Effects 0.000 claims 9
- 235000018102 proteins Nutrition 0.000 claims 9
- 102000004169 proteins and genes Human genes 0.000 claims 9
- 108090000623 proteins and genes Proteins 0.000 claims 9
- 230000035772 mutation Effects 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 7
- 229940079593 drugs Drugs 0.000 claims 7
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 6
- 102100011432 CRKL Human genes 0.000 claims 5
- 101700072217 CRKL Proteins 0.000 claims 5
- 206010025650 Malignant melanoma Diseases 0.000 claims 5
- 238000004113 cell culture Methods 0.000 claims 5
- 210000004748 cultured cells Anatomy 0.000 claims 5
- 201000001441 melanoma Diseases 0.000 claims 5
- 101700025368 ERBB2 Proteins 0.000 claims 4
- 102000027760 ERBB2 Human genes 0.000 claims 4
- 101710038831 PRKCE Proteins 0.000 claims 4
- 101710038847 PRKCH Proteins 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 238000002648 combination therapy Methods 0.000 claims 4
- 108020004707 nucleic acids Proteins 0.000 claims 4
- 150000007523 nucleic acids Chemical class 0.000 claims 4
- 235000001014 amino acid Nutrition 0.000 claims 3
- 150000001413 amino acids Chemical group 0.000 claims 3
- YABJJWZLRMPFSI-UHFFFAOYSA-N 1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl]oxy-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine Chemical group N=1C2=CC(OC=3C=C(N=CC=3)C=3NC(=CN=3)C(F)(F)F)=CC=C2N(C)C=1NC1=CC=C(C(F)(F)F)C=C1 YABJJWZLRMPFSI-UHFFFAOYSA-N 0.000 claims 2
- PYEFPDQFAZNXLI-UHFFFAOYSA-N 3-(dimethylamino)-N-[3-[(4-hydroxybenzoyl)amino]-4-methylphenyl]benzamide Chemical compound CN(C)C1=CC=CC(C(=O)NC=2C=C(NC(=O)C=3C=CC(O)=CC=3)C(C)=CC=2)=C1 PYEFPDQFAZNXLI-UHFFFAOYSA-N 0.000 claims 2
- 108060000207 AK3 Proteins 0.000 claims 2
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 206010018338 Glioma Diseases 0.000 claims 2
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- DPCXEUSDRQOOGZ-QLYXXIJNSA-N N,N-dimethyl-2-[4-[(4Z)-4-(1-nitroso-2,3-dihydroinden-5-ylidene)-5-(1H-pyridin-4-ylidene)-1H-imidazol-2-yl]phenoxy]ethanamine Chemical compound C1=CC(OCCN(C)C)=CC=C1C(NC1=C2C=CNC=C2)=N\C1=C\1C=C2CCC(N=O)=C2C=C/1 DPCXEUSDRQOOGZ-QLYXXIJNSA-N 0.000 claims 2
- YZDJQTHVDDOVHR-UHFFFAOYSA-N N-{3-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl}propane-1-sulfonamide Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(Cl)=CN=C3NC=2)=C1F YZDJQTHVDDOVHR-UHFFFAOYSA-N 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 102100008310 PAK3 Human genes 0.000 claims 2
- 101700076719 PAK3 Proteins 0.000 claims 2
- -1 PD334581 Chemical compound 0.000 claims 2
- 102100016970 PRKCE Human genes 0.000 claims 2
- 102100019669 PRKCH Human genes 0.000 claims 2
- 101710007825 RNASE3 Proteins 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 201000011231 colorectal cancer Diseases 0.000 claims 2
- 230000014509 gene expression Effects 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 230000002018 overexpression Effects 0.000 claims 2
- 229920001184 polypeptide Polymers 0.000 claims 2
- 229960003787 sorafenib Drugs 0.000 claims 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 claims 2
- 229960003862 vemurafenib Drugs 0.000 claims 2
- LFTHSVHVSCMOQP-UHFFFAOYSA-N 6-methoxy-7-(3-morpholin-4-ylpropoxy)-4-(4-phenoxyanilino)quinoline-3-carbonitrile Chemical compound N#CC1=CN=C2C=C(OCCCN3CCOCC3)C(OC)=CC2=C1NC(C=C1)=CC=C1OC1=CC=CC=C1 LFTHSVHVSCMOQP-UHFFFAOYSA-N 0.000 claims 1
- DEZZLWQELQORIU-RELWKKBWSA-N GDC-0879 Chemical compound N=1N(CCO)C=C(C=2C=C3CCC(/C3=CC=2)=N\O)C=1C1=CC=NC=C1 DEZZLWQELQORIU-RELWKKBWSA-N 0.000 claims 1
- 229960002989 Glutamic Acid Drugs 0.000 claims 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 1
- RDSACQWTXKSHJT-NSHDSACASA-N N-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide Chemical compound C1CC1(C[C@H](O)CO)S(=O)(=O)NC=1C(OC)=CC(F)=C(F)C=1NC1=CC=C(I)C=C1F RDSACQWTXKSHJT-NSHDSACASA-N 0.000 claims 1
- CYOHGALHFOKKQC-UHFFFAOYSA-N Selumetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1Cl CYOHGALHFOKKQC-UHFFFAOYSA-N 0.000 claims 1
- 230000001747 exhibiting Effects 0.000 claims 1
- 229910021526 gadolinium-doped ceria Inorganic materials 0.000 claims 1
- 235000013922 glutamic acid Nutrition 0.000 claims 1
- 239000004220 glutamic acid Substances 0.000 claims 1
- VLCMRTMCMQJSKM-UHFFFAOYSA-N phenyl-[4-phenyl-8-(trifluoromethyl)quinolin-3-yl]methanone Chemical compound C=1C=CC=CC=1C(=O)C1=CN=C2C(C(F)(F)F)=CC=CC2=C1C1=CC=CC=C1 VLCMRTMCMQJSKM-UHFFFAOYSA-N 0.000 claims 1
- 230000001177 retroviral Effects 0.000 claims 1
- 239000004474 valine Substances 0.000 claims 1
- 230000035899 viability Effects 0.000 claims 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31219310P | 2010-03-09 | 2010-03-09 | |
| US61/312,193 | 2010-03-09 | ||
| US31251910P | 2010-03-10 | 2010-03-10 | |
| US61/312,519 | 2010-03-10 | ||
| US32602110P | 2010-04-20 | 2010-04-20 | |
| US61/326,021 | 2010-04-20 | ||
| US41556910P | 2010-11-19 | 2010-11-19 | |
| US61/415,569 | 2010-11-19 | ||
| PCT/US2011/027689 WO2011112678A1 (en) | 2010-03-09 | 2011-03-09 | Methods of diagnosing and treating cancer in patients having or developing resistance to a first cancer therapy |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013526843A JP2013526843A (ja) | 2013-06-27 |
| JP2013526843A5 true JP2013526843A5 (pt) | 2014-04-24 |
| JP5985401B2 JP5985401B2 (ja) | 2016-09-06 |
Family
ID=43837946
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012557201A Active JP5985401B2 (ja) | 2010-03-09 | 2011-03-09 | 第一の癌療法に対する耐性を現に有するか、または、そのような耐性を生じる患者において癌を診断および治療する方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US20130059851A1 (pt) |
| EP (1) | EP2545187B1 (pt) |
| JP (1) | JP5985401B2 (pt) |
| KR (1) | KR20120139767A (pt) |
| CN (1) | CN103038364A (pt) |
| AU (1) | AU2011224410B2 (pt) |
| BR (1) | BR112012022801B8 (pt) |
| CA (1) | CA2791247C (pt) |
| EA (1) | EA030276B1 (pt) |
| ES (1) | ES2714875T3 (pt) |
| MX (1) | MX343368B (pt) |
| WO (1) | WO2011112678A1 (pt) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
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| TWI535445B (zh) | 2010-01-12 | 2016-06-01 | 安可美德藥物股份有限公司 | Ｗｎｔ拮抗劑及治療和篩選方法 |
| MX347515B (es) | 2010-04-01 | 2017-04-28 | Oncomed Pharmaceuticals Inc * | Agentes que se unen al receptor encrespado y usos de los mismos. |
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| US10202643B2 (en) | 2011-10-31 | 2019-02-12 | University Of Utah Research Foundation | Genetic alterations in glioma |
| JP2015502958A (ja) * | 2011-12-09 | 2015-01-29 | オンコメッド ファーマシューティカルズ インコーポレイテッド | がんの処置のための併用療法 |
| PL2831589T3 (pl) * | 2012-03-28 | 2018-10-31 | Dana-Farber Cancer Institute, Inc. | Mutanty C-RAF, które nadają oporność na inhibitory RAF |
| EP2884979B1 (en) | 2012-08-17 | 2019-06-26 | F.Hoffmann-La Roche Ag | Combination therapies for melanoma comprising administering cobimetinib and vemurafinib |
| EP2911691B1 (en) | 2012-10-23 | 2018-10-10 | OncoMed Pharmaceuticals, Inc. | Methods of treating neuroendocrine tumors using wnt pathway-binding agents |
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| KR20160129609A (ko) | 2015-04-30 | 2016-11-09 | 삼성전자주식회사 | Ｂｒａｆ 저해제를 포함하는 세포 또는 개체의 노화를 감소시키기 위한 조성물 및 그의 용도 |
| US9815818B2 (en) | 2015-07-06 | 2017-11-14 | Gilead Sciences, Inc. | Cot modulators and methods of use thereof |
| CA2971640C (en) | 2015-07-06 | 2020-09-22 | Gilead Sciences, Inc. | Cot modulators and methods of use thereof |
| GB201520178D0 (en) * | 2015-11-16 | 2015-12-30 | Univ London Queen Mary | Method |
| CN105695616A (zh) * | 2016-04-22 | 2016-06-22 | 王冬国 | 诊断甲状腺癌的分析标志物及其应用 |
| WO2018005435A1 (en) | 2016-06-30 | 2018-01-04 | Gilead Sciences, Inc. | 4,6-diaminoquinazolines as cot modulators and methods of use thereof |
| WO2018027223A1 (en) * | 2016-08-05 | 2018-02-08 | Duke University | Camkk2 inhibitor compositions and methods of using the same |
| EP3559276B1 (en) | 2016-12-20 | 2022-03-23 | ETH Zurich | Identification of drugs targeting non-genetic drug tolerance programs in cancer |
| US10793901B2 (en) * | 2016-12-28 | 2020-10-06 | Roche Molecular Systems, Inc. | Reversibly protected nucleotide reagents with high thermal stability |
| JP7300394B2 (ja) | 2017-01-17 | 2023-06-29 | ヘパリジェニックス ゲーエムベーハー | 肝再生の促進又は肝細胞死の低減もしくは予防のためのプロテインキナーゼ阻害 |
| WO2019090020A1 (en) * | 2017-11-02 | 2019-05-09 | University Of Georgia Research Foundation, Inc. | Methods and compositions related to increased rotavirus production |
| CN108872438B (zh) * | 2018-08-06 | 2021-01-15 | 杭州迪相实业有限公司 | 一种外泌体中肺癌标志物gk5快速检测试剂盒 |
| US20230183204A9 (en) * | 2018-11-07 | 2023-06-15 | Dana-Farber Cancer Institute, Inc. | Benzimidazole derivatives and aza-benzimidazole derivatives as janus kinase 2 inhibitors and uses thereof |
| EP3931564A4 (en) * | 2019-02-26 | 2023-04-26 | Cell Response, Inc. | METHODS OF TREATMENT OF MAP3K8 POSITIVE TUMORS |
| TW202235416A (zh) | 2019-06-14 | 2022-09-16 | 美商基利科學股份有限公司 | Cot 調節劑及其使用方法 |
| CN110862968A (zh) * | 2019-10-30 | 2020-03-06 | 中国农业科学院兰州兽医研究所 | Map3k8基因敲除pk-15细胞系的构建方法及其应用 |
| KR20220161438A (ko) | 2020-03-30 | 2022-12-06 | 길리애드 사이언시즈, 인코포레이티드 | Cot 억제제 화합물, (S)-6-(((1-(바이사이클로[1.1.1]펜탄-1-일)-1H-1,2,3-트라이아졸-4-일)2-메틸-1-옥소-1,2-다이하이드로아이소퀴놀린-5-일)메틸)))아미노8-클로로-(네오펜틸아미노)퀴놀린-3-카르보니트릴의 고체 형태 |
| WO2021202688A1 (en) | 2020-04-02 | 2021-10-07 | Gilead Sciences, Inc. | Process for preparing a cot inhibitor compound |
| AU2021267373A1 (en) | 2020-05-06 | 2022-12-08 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors |
| WO2022140527A1 (en) | 2020-12-23 | 2022-06-30 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| EP4430042A1 (en) | 2021-11-09 | 2024-09-18 | Ajax Therapeutics, Inc. | 6-he tero aryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
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- 2011-03-09 KR KR1020127025801A patent/KR20120139767A/ko active IP Right Grant
- 2011-03-09 CN CN2011800231091A patent/CN103038364A/zh active Pending
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